dBET57
Based on 4 publication(s) in Google Scholar
dBET57 is an effective and selective BRD4BD1 degrader based on PROTAC technology, with the ability to induce cell apoptosis and anti-tumor activity. dBET57 mediates the recruitment of the E3 ubiquitin ligase CRL4Cereblon, showing a DC50/5h value of 500 nM for BRD4BD1.
(Pink: BRD4BD1 ligand (HY-78695); Blue: Cereblon ligand (HY-10984); Black: linker).
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.94%
- CAS 番号: 1883863-52-2
- 分子式: C34H31ClN8O5S
- 分子量:699.18
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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BRD4 (BD1) 500 nM (DC50) |
dBET57 (0-10000 nM, 72 h) inhibits the proliferation of NB cells, with the IC50 values for SK-N-BE(2), IMR-32, SH-SY5Y, HT22, HPAEC, 293T, HCAEC being 643.4, 299, 414, 2151, 2321, 4840 and 3939 nM[1].
dBET57 (0-1200 nM, 48 h) induces apoptosis in NB cells, and increases the proportion of cells in the G1 phase[1].
dBET57 (0-1200 nM, 0-48 h) reduces the migration and adhesion capabilities of NB cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SK-N-BE(2), IMR-32, SH-SY5Y, HT22, HPAEC, 293T, HCAEC
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Concentration:0-10000 nM
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Incubation Time:48 h
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Result:Inhibited NB cell proliferation.
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Cell Line:SK-NBE(2), IMR-32, SH-SY5Y
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Concentration:0, 300, 600, 1200 nM
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Incubation Time:48 h
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Result:Increased PARP activation in a dose-dependent manner, while Bcl-2 expression gradually decreased, reduced the expression of BRD4, BRD2, BRD3, and N-Myc.
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Cell Line:SK-NBE(2), IMR-32, SH-SY5Y
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Concentration:0, 300, 600, 1200 nM
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Incubation Time:48 h
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Result:Increased apoptosis rate in a dose-dependent manner.
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Cell Line:SK-NBE(2), IMR-32, SH-SY5Y
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Concentration:0, 300, 600, 1200 nM
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Incubation Time:72 h
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Result:Increased the proportion of NB cells in G1 phase and decreased the proportion of NB cells in G2 and S phase.
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Cell Line:SK-NBE(2), IMR-32, SH-SY5Y
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Concentration:0, 1200 nM
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Incubation Time:48 h
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Result:Reduced cell migration.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SK-NBE(2) xenograft mouse model[1]
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Dosage:7.5 mg/kg, daily, 2 weeks
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Administration:Intraperitoneal injection (i.p.)
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Result:Reduced tumor volume, decreased the proportion of ki-67 positive cells, increased the proportion of caspase3, had no obvious organ toxicity, and downregulated the level of ZMYND8.
化学情報
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CAS 番号 1883863-52-2
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性状 Solid
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分子量 699.18
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分子式 C34H31ClN8O5S
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Color Light yellow to yellow
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SMILES
O=C(NCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)C[C@H]4C5=NN=C(C)N5C6=C(C(C)=C(C)S6)C(C7=CC=C(Cl)C=C7)=N4
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (4)
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Journal Impact Factor
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Most Recent
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Nat Chem Biol
2023 Mar;19(3):323-333. PMID: 36329119 -
Adv Healthc Mater
Golgi Apparatus-Targeting Immunostimulant for Synergistic Activation of Antitumor Immunity via Pyroptosis Induction and PD-L1 Degradation. [Abstract]2026 Feb 17:e04895. PMID: 41700108 -
Structure
PROTAC-mediated activation, rather than degradation, of a nuclear receptor reveals complex ligand-receptor interaction network. [Abstract]2024 Dec 5;32(12):2352-2363.e8. PMID: 39389062 -
Biochem Biophys Res Commun
Accelerating PROTAC drug discovery: Establishing a relationship between ubiquitination and target protein degradation. [Abstract]2022 Nov 5:628:68-75. PMID: 36084553
溶剤 & 溶解度
DMSO : 250 mg/mL (357.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (2.97 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (283 KB)
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SDS (396 KB)
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- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
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- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Si-Qi Jia, et al. The BRD4 Inhibitor dBET57 Exerts Anticancer Effects by Targeting Superenhancer-Related Genes in Neuroblastoma. J Immunol Res. 2022 Nov 16:2022:7945884. [Content Brief]
[2]. Nowak RP, et al. Plasticity in binding confers selectivity in ligand-induced protein degradation. Nat Chem Biol. 2018 Jul;14(7):706-714. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.4302 mL | 7.1512 mL | 14.3025 mL | 35.7562 mL |
| 5 mM | 0.2860 mL | 1.4302 mL | 2.8605 mL | 7.1512 mL | |
| 10 mM | 0.1430 mL | 0.7151 mL | 1.4302 mL | 3.5756 mL | |
| 15 mM | 0.0953 mL | 0.4767 mL | 0.9535 mL | 2.3837 mL | |
| 20 mM | 0.0715 mL | 0.3576 mL | 0.7151 mL | 1.7878 mL | |
| 25 mM | 0.0572 mL | 0.2860 mL | 0.5721 mL | 1.4302 mL | |
| 30 mM | 0.0477 mL | 0.2384 mL | 0.4767 mL | 1.1919 mL | |
| 40 mM | 0.0358 mL | 0.1788 mL | 0.3576 mL | 0.8939 mL | |
| 50 mM | 0.0286 mL | 0.1430 mL | 0.2860 mL | 0.7151 mL | |
| 60 mM | 0.0238 mL | 0.1192 mL | 0.2384 mL | 0.5959 mL | |
| 80 mM | 0.0179 mL | 0.0894 mL | 0.1788 mL | 0.4470 mL | |
| 100 mM | 0.0143 mL | 0.0715 mL | 0.1430 mL | 0.3576 mL |
dBET57 関連分類
HY-123844 関連分類
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